Chemical Structure : BAY 2402234
CAS No.: 2225819-06-5
货号: PC-36161Not For Human Use, Lab Use Only.
BAY 2402234 (BAY2402234) is a novel potent, selective, orally bioavailable DHODH inhibitor with IC50 of 1.2 nM (human full-length DHODH).
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---|---|---|---|
5 mg | ¥3880 | In stock | |
10 mg | ¥5980 | In stock | |
25 mg | ¥9880 | In stock | |
50 mg | Get quote | ||
100 mg | Get quote |
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Orludodstat (BAY2402234) is a novel potent, selective, orally bioavailable DHODH inhibitor with IC50 of 1.2 nM (human full-length DHODH).
BAY2402234 binds the ubiquinone binding site of DHODH between the N-terminal helices.
BAY2402234 causes dose-dependent upregulation of CD11b with EC50s of 3.16 nM in MOLM-13 cells and 0.96 nM in HEL cells, inhibits the proliferation of THP-1 cells with an IC50 of 2.6 nM, as well as nine other leukemia cell lines representing diverse AML subtypes (IC50=0.08-8.2 nM).
BAY 2402234 shows monotherapy efficacy and differentiation induction across multiple AML subtypes both in vitro and in vivo.
分子量 | 520.841 | |
分子式 | C21H18ClF5N4O4 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
(S)-N-(2-chloro-6-fluorophenyl)-4-(4-ethyl-3-(hydroxymethyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)-5-fluoro-2-((1,1,1-trifluoropropan-2-yl)oxy)benzamide |
1. Christian S, et al. Leukemia. 2019 Apr 2. doi: 10.1038/s41375-019-0461-5.
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